DESIGN, SYNTHESIS, AND ANTITUMOR ACTIVITY-ABSOLUTE CONFIGURATION RELATIONSHIPS OF PODOPHYLLOTOXIN AZA-ANALOGS

DESIGN, SYNTHESIS, AND ANTITUMOR ACTIVITY-ABSOLUTE CONFIGURATION RELATIONSHIPS OF PODOPHYLLOTOXIN AZA-ANALOGS
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DOI:
10.1016/s0040-4020(01)80545-7
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发表时间:
1993-02-26
期刊:
影响因子:
2.1
通讯作者:
KOGA, K
KOGA, K
中科院分区:
化学3区
文献类型:
--
作者:
TOMIOKA, K;KUBOTA, Y;KOGA, K

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通过环脲烷10或16与3,4,5-三甲氧基苯甲醛11的高度立体选择性缩合反应,设计并合成了具有光学活性和外消旋性的鬼臼毒素aza类似物3约7,并发现其具有良好的体外和体内抗肿瘤活性。
Optically active and racemic podophyllotoxin aza-analogues 3 approximately 7 were designed and synthesized by a highly stereoselective condensation reaction of a cyclic urethane 10 or 16 with 3,4,5-trimethoxybenzaldehyde 11 and were found to show a promising in vitro and in vivo antitumor activity.